EGFR-IN-172
EGFR-IN-172 is a EGFR inhibitor. EGFR-IN-172 effectively inhibits the proliferation of non-small cell lung cancer (NSCLC) cells carrying the L858R, T790M and C797S drug-resistant mutations. EGFR-IN-172 inhibits EGFR phosphorylation, induces cell cycle arrest and apoptosis. EGFR-IN-172 can be used for the study of NSCLC.
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- CAS No.: 878416-74-1
- Formule: C22H18FN3O
- Masse moléculaire:359.40
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-87MG ATCC | IC50 |
9.2 μM
Compound: CD373
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Cytotoxicity against human U-87 MG cells assessed as growth inhibition measured after 72 hrs by MTT assay
Cytotoxicity against human U-87 MG cells assessed as growth inhibition measured after 72 hrs by MTT assay
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[PMID: 32830969] |
In Vitro
EGFR-IN-172 (Compound 2b) shows high antiproliferative activity against A549 cells (EGFRWT) (IC50 = 5.31 μM), PC-9 cell (EGFRT790M) (IC50 = 0.55 μM), H1975 cells (EGFRL858R/T790M) (IC50 = 0.40 μM) and Ba/F3-EGFRL858R/T790M/C797S cells (IC50 = 2.36 μM)[1].
EGFR-IN-172 (0.1-10 μM) inhibits the phosphorylation of EGFR (pEGFR) in H1975 and Ba/F3 triple-mutant cells in a concentration-dependent manner[1].
EGFR-IN-172 (0.25-1 μM, 48 h) arrests the H1975 cells in the G0/G1 phase, but has no significant effect on the cell cycle of the Ba/F3 triple-mutant cells[1].
EGFR-IN-172 (0.25-1 μM, 48 h) induces apoptosis in H1975 and Ba/F3 triple-mutant cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1975 and Ba/F3-EGFRL858R/T790M/C797S cells
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Concentration:0.25, 0.5 and 1 μM
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Incubation Time:48 h
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Result:Arrested H1975 cells in the G0/G1 phase of the cell cycle.
Did not affect Ba/F3-EGFRL858R/T790M/C797S cells.
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Cell Line:H1975 and Ba/F3-EGFRL858R/T790M/C797S cells
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Concentration:0.25, 0.5 and 1 μM
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Incubation Time:48 h
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Result:Effectively induced apoptosis in two EGFR mutant lung cancer cells.
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Cell Line:H1975 and Ba/F3-EGFRL858R/T790M/C797S cells
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Concentration:0.25, 0.5 and 1 μM
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Incubation Time:48 h
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Result:Inhibited the phosphorylation of EGFR in a concentration-dependent manner in both cell lines.
- Kinase activity and phosphorylation assays
- Western Blot
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Protocol for Kinase activity and phosphorylation assays
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 878416-74-1
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Masse moléculaire 359.40
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Formule C22H18FN3O
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SMILES
OC1=C2N=CC=CC2=CC=C1C(C3=CC=CC(F)=C3)NC4=NC=CC(C)=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR-IN-172 Related Classifications
HY-175837 Related Classifications
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